盐酸多柔比星脂质体的制备及体外释放研究
Preparation and in vitro Release of Doxorubicin Hydrochloride Liposome
王秋云 1岳占国 1潘颖彬1
作者信息
- 1. 广州玻思韬控释药业有限公司,广东广州 510530
- 折叠
摘要
目的 制备盐酸多柔比星脂质体(DOX-Lip),并研究其体外释放行为.方法 采用硫酸铵梯度法制备DOX-Lip,通过单因素考察硫酸铵溶液pH、油水比、挤出次数、超滤次数、孵育温度和时间对DOX-Lip包封率的影响.再以包封率为评价指标,采用正交试验进行处方工艺优化,并评价其体外释放行为.结果 经最优处方工艺制备的DOX-Lip为类圆球形,分布均匀.平均粒径为85 nm～87 nm(PDI =0.052～0.078),Zeta电位为-15 mV～-16 mV,包封率为96%～97%.体外释放与市售参比制剂相似,具有明显的缓释性.结论 采用最优处方工艺制备DOX-Lip稳定可行,具有明显的缓释特征,体外释放与参比制剂相似,为该产品的生物等效性评价提供研究基础.
Abstract
OBJECTIVE To prepare doxorubicin hydrochloride liposome(DOX-Lip)and investigate its in vitro release behavior.METHODS DOX-Lip was prepared by ammonium sulfate gradient methods.The encapsulation ef-ficiency of doxorubicin were investigated by a single factor of ammonium sulfate pH,oil to water ratio,extrusion pas-ses,diafiltration passes,incubation temperature and duration.Taking encapsulation efficiency as evaluation indica-tors,the orthogonal test was used to optimize the formulation process of DOX-Lip and investigate in vitro release be-havior.RESULTS DOX-Lip which prepared by optimal formulation process was spherical with a uniform size distri-bution.The particle size was 85 nm-87 nm(PDI =0.052-0.078),the Zeta potential was-15 mV--16 mV and the encapsulation efficiency was 96%-97%.DOX-Lip released slowly in vitro and was similar to that of the ref-erence listed drug(RLD).CONCLUSION DOX-Lip prepared by the optimal formulation process is stable and feasible,has obvious sustained-release characteristics and is similar to that of RLD,and provides a research basis for the bioequivalence evaluation of doxorubicin hydrochloride liposome injection.
关键词
盐酸多柔比星/脂质体/正交试验/体外释放Key words
Doxorubicin hydrochloride/Liposomes/Orthogonal test/in vitro drug release引用本文复制引用
出版年
2024
NETL
NSTL
万方数据